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The following message was posted to: PharmPK
Does anybody happen to know the IC50 or Ki values of venlafaxine and
duloxetine in vitro (human liver microsomes)?
Kind regards,
Morten Priskorn
(mp.-at-.neurosearch.dk)
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The following message was posted to: PharmPK
Dear Morten,
It looks like that venlafaxine has a low potential to inhibit the
metabolism
of substrates for CYP2D6 such as imipramine and desipramine, but does
not
inhibit ethoxyresorufin O-dealkylase (CYP1A2), tolbutamide 4-hydroxylase
(CYP2C9) or testosterone 6 beta-hydroxylase (CYP3A4) activities at
concentrations of up to 1 mM (see refs below by Ball SE, Ahern D,
Scatina J,
Kao J.
Venlafaxine: in vitro inhibition of CYP2D6 dependent imipramine and
desipramine metabolism; comparative studies with selected SSRIs, and
effects
on human hepatic CYP3A4, CYP2C9 and CYP1A2. Br J Clin Pharmacol. 1997
Jun;43(6):619-26).
Here are some other refs that may also prove helpful:
von Moltke LL, Duan SX, Greenblatt DJ, Fogelman SM, Schmider J,
Harmatz
JS,
Shader RI.
Venlafaxine and metabolites are very weak inhibitors of human
cytochrome
P450-3A isoforms.
Biol Psychiatry. 1997 Feb 1;41(3):377-80. No abstract available.
PMID: 9024962 [PubMed - indexed for MEDLINE]
von Moltke LL, Greenblatt DJ, Duan SX, Schmider J, Kudchadker L,
Fogelman
SM, Harmatz JS, Shader RI.
Phenacetin O-deethylation by human liver microsomes in vitro:
inhibition by
chemical probes, SSRI antidepressants, nefazodone and venlafaxine.
Psychopharmacology (Berl). 1996 Dec;128(4):398-407.
PMID: 8986010 [PubMed - indexed for MEDLINE]
Otton SV, Ball SE, Cheung SW, Inaba T, Rudolph RL, Sellers EM.
Venlafaxine oxidation in vitro is catalysed by CYP2D6.
Br J Clin Pharmacol. 1996 Feb;41(2):149-56.
PMID: 8838442 [PubMed - indexed for MEDLINE]
Kishore
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